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Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction
Opioid-induced bowel dysfunction (OIBD) is a burdensome condition which limits the therapeutic benefit of analgesia. It affects the entire gastrointestinal tract, predominantly by activating opioid receptors in the enteric nervous system, resulting in a wide range of symptoms, such as reflux, bloati...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4179399/ https://www.ncbi.nlm.nih.gov/pubmed/25278772 http://dx.doi.org/10.2147/CEG.S52097 |
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author | Poulsen, Jakob Lykke Brock, Christina Olesen, Anne Estrup Nilsson, Matias Drewes, Asbjørn Mohr |
author_facet | Poulsen, Jakob Lykke Brock, Christina Olesen, Anne Estrup Nilsson, Matias Drewes, Asbjørn Mohr |
author_sort | Poulsen, Jakob Lykke |
collection | PubMed |
description | Opioid-induced bowel dysfunction (OIBD) is a burdensome condition which limits the therapeutic benefit of analgesia. It affects the entire gastrointestinal tract, predominantly by activating opioid receptors in the enteric nervous system, resulting in a wide range of symptoms, such as reflux, bloating, abdominal cramping, hard, dry stools, and incomplete evacuation. The majority of studies evaluating OIBD focus on constipation experienced in approximately 60% of patients. Nevertheless, other presentations of OIBD seem to be equally frequent. Furthermore, laxative treatment is often insufficient, which in many patients results in decreased quality of life and discontinuation of opioid treatment. Novel mechanism-based pharmacological approaches targeting the gastrointestinal opioid receptors have been marketed recently and even more are in the pipeline. One strategy is prolonged release formulation of the opioid antagonist naloxone (which has limited systemic absorption) and oxycodone in a combined tablet. Another approach is peripherally acting, μ-opioid receptor antagonists (PAMORAs) that selectively target μ-opioid receptors in the gastrointestinal tract. However, in Europe the only PAMORA approved for OIBD is the subcutaneously administered methylnaltrexone. Alvimopan is an oral PAMORA, but only approved in the US for postoperative ileus in hospitalized patients. Finally, naloxegol is a novel, oral PAMORA expected to be approved soon. In this review, the prevalence and pathophysiology of OIBD is presented. As PAMORAs seem to be a promising approach, their potential effect is reviewed with special focus on naloxegol’s pharmacological properties, data on safety, efficacy, and patient-focused perspectives. In conclusion, as naloxegol is administered orally once daily, has proven efficacious compared to placebo, has an acceptable safety profile, and can be used as add-on to existing pain treatment, it is a welcoming addition to the targeted treatment possibilities for OIBD. |
format | Online Article Text |
id | pubmed-4179399 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-41793992014-10-02 Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction Poulsen, Jakob Lykke Brock, Christina Olesen, Anne Estrup Nilsson, Matias Drewes, Asbjørn Mohr Clin Exp Gastroenterol Review Opioid-induced bowel dysfunction (OIBD) is a burdensome condition which limits the therapeutic benefit of analgesia. It affects the entire gastrointestinal tract, predominantly by activating opioid receptors in the enteric nervous system, resulting in a wide range of symptoms, such as reflux, bloating, abdominal cramping, hard, dry stools, and incomplete evacuation. The majority of studies evaluating OIBD focus on constipation experienced in approximately 60% of patients. Nevertheless, other presentations of OIBD seem to be equally frequent. Furthermore, laxative treatment is often insufficient, which in many patients results in decreased quality of life and discontinuation of opioid treatment. Novel mechanism-based pharmacological approaches targeting the gastrointestinal opioid receptors have been marketed recently and even more are in the pipeline. One strategy is prolonged release formulation of the opioid antagonist naloxone (which has limited systemic absorption) and oxycodone in a combined tablet. Another approach is peripherally acting, μ-opioid receptor antagonists (PAMORAs) that selectively target μ-opioid receptors in the gastrointestinal tract. However, in Europe the only PAMORA approved for OIBD is the subcutaneously administered methylnaltrexone. Alvimopan is an oral PAMORA, but only approved in the US for postoperative ileus in hospitalized patients. Finally, naloxegol is a novel, oral PAMORA expected to be approved soon. In this review, the prevalence and pathophysiology of OIBD is presented. As PAMORAs seem to be a promising approach, their potential effect is reviewed with special focus on naloxegol’s pharmacological properties, data on safety, efficacy, and patient-focused perspectives. In conclusion, as naloxegol is administered orally once daily, has proven efficacious compared to placebo, has an acceptable safety profile, and can be used as add-on to existing pain treatment, it is a welcoming addition to the targeted treatment possibilities for OIBD. Dove Medical Press 2014-09-19 /pmc/articles/PMC4179399/ /pubmed/25278772 http://dx.doi.org/10.2147/CEG.S52097 Text en © 2014 Poulsen et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Review Poulsen, Jakob Lykke Brock, Christina Olesen, Anne Estrup Nilsson, Matias Drewes, Asbjørn Mohr Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
title | Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
title_full | Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
title_fullStr | Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
title_full_unstemmed | Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
title_short | Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
title_sort | clinical potential of naloxegol in the management of opioid-induced bowel dysfunction |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4179399/ https://www.ncbi.nlm.nih.gov/pubmed/25278772 http://dx.doi.org/10.2147/CEG.S52097 |
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